0.1%他克莫司软膏的体外透皮吸收研究
The Transdermal Research of 0.1%Tacrolimus Ointment
肖学成 1张磊 1彭秀菊 1熊驰1
作者信息
- 1. 湖北中医药大学药学院 武汉 430065
- 折叠
摘要
目的：建立0.1%他克莫司软膏体外透皮接收液中药物的HPLC测定方法，研究0.1%他克莫司软膏的体外透皮量。方法：采用Kromasil 100-5 C18色谱柱（250mm×4.6mm，5μm）；流动相：乙腈-水-磷酸（690∶310∶1）；流速：1.0ml/min；检测波长：215nm。体外透皮实验采用自制改良的Franz直立式扩散池，使用实验用离体乳猪皮作为透皮屏障。将自制凝胶与市售凝胶的透皮结果进行对比分析，分别在设定的1h、2h、4h、6h、8h、12h时间点取样测定透皮接收液中他克莫司的浓度，计算累积透皮量。结果：他克莫司的标准曲线方程为A=17408.1203×C+555.4604（r=0.9995），线性范围为2.036～20.36μg/ml，平均回收率为99.15%。结果表明，累积透皮量与时间呈现良好的线性关系，自制乳膏与市售乳膏的透皮结果无显著性差异（P＞0.05）。结论：本检测方法操作简便，快速准确，是考察他克莫司软膏的体外透皮性能比较理想的方法。
Abstract
Objective:To establish an HPLC method for quantitative the determination of tacrolimus in vitro percutaneous solution,and investigate the ability of percutaneous penetration of 0.1% tacrolimus ointment. Methods:Kromasil 100-5 C18 column (250mm × 4.6mm,5μm)was used as the fixed phase and a mixture of acetonitrile,purified water and phosphoric acid (690∶310∶1) as mobile phase.The flow rate was 1.0 ml/min.The detection wavelength was 215nm.Improved Franz type diffusion cells were used in vitro permeation studies and excised minipigs skins in vitro were used as transdermal barrier.The concentration of 0.1% tacrolimus ointment in the receptor solution was determined by HPLC to investigate its cumulative permeation quantities at different time respectively and compared with that of the commercial ointment. Results:The regression equation of tacrolimus ointment was linear in the range of 2.036~20.36μg/ml A=17408.1203×C+555.4604 (r=0.9995).The average recovery was 99.15%.A good linear relationship existed between the cumulative penetration quantities and the time.There was no significant difference in the permeation quantities between the self-made and commercial ointment. Conclusion:The method was simple, rapid, and accurate. It is a good method to evaluate the characteristic of permeation for tacrolimus ointment.
关键词
0.1%他克莫司软膏/体外透皮吸收/高效液相色谱法Key words
0.1%Tacrolimus/Ointment/Percutaneous absorption/HPLC引用本文复制引用
出版年
2014
NETL
NSTL
维普
万方数据